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Selective Degradation Of Cdk6 By A Palbociclib Based
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A Potent And Selective Small-Molecule Degrader Of Stat3
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Proteolysis-Targeting Chimeras As Therapeutics And
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Senescence-Induced Vascular Remodeling Creates
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Small Extracellular Vesicles Are Key Regulators Of
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Homolog-Selective Degradation As A Strategy To Probe
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Cell Chemical Biology |
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Eed-Targeted Protacs Degrade Eed, Ezh2, And Suz12 In
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Cell Chemical Biology |
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Degradation Of Polycomb Repressive Complex 2 With An
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Cell Chemical Biology |
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Exploring Targeted Degradation Strategy For Oncogenic
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Cell Chemical Biology |
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Protacs: An Emerging Therapeutic Modality In Precision
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Cell Chemical Biology |
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Obesity-Induced Cellular Senescence Drives Anxiety And
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Targeted Elimination Of Senescent Beta Cells Prevents
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Cell Metabolism |
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Bivalent Ligands For Protein Degradation In Drug
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Computational And Structural Biotechnology Journal |
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10.1016/j.ctrv.2020.101974 |
Kras G12C Game Of Thrones, Which Direct Kras Inhibitor
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10.1016/j.ddtec.2018.12.002 |
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Drug Discovery Today: Technologies |
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10.1016/j.ebiom.2018.09.005 |
Small-Molecule Protacs: An Emerging And Promising
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An, Sainan; Fu, Liwu |
Ebiomedicine |
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Fisetin Is A Senotherapeutic That Extends Health And
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Ebiomedicine |
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Senolytics In Idiopathic Pulmonary Fibrosis: Results
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Ebiomedicine |
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10.1016/j.ebiom.2019.01.056 |
Senolytics And Senostatics As Adjuvant Tumour
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Ebiomedicine |
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10.1016/j.ebiom.2019.08.069 |
Senolytics Decrease Senescent Cells In Humans:
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Hickson, Latonya J.; Langhi Prata, Larissa G.P.;
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K.; Herrmann, Sandra M.; Jensen, Michael D.; Jia, Qingyi; Jordan, Kyra
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Ebiomedicine |
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10.1016/j.molcel.2019.09.009 |
Autacs: Cargo-Specific Degraders Using Selective
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Takahashi, Daiki; Moriyama, Jun; Nakamura, Tomoe; Miki,
Erika; Takahashi, Eriko; Sato, Ayami; Akaike, Takaaki; Itto-Nakama,
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Molecular Cell |
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10.1016/j.molcel.2020.01.010 |
Harnessing The Power Of Proteolysis For Targeted
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Verma, Rati; Mohl, Dane; Deshaies, Raymond J. |
Molecular Cell |
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10.1016/j.smim.2019.04.003 |
Senescent Cell Clearance By The Immune System: Emerging
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Prata, Larissa G.P. Langhi; Ovsyannikova, Inna G.;
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10.1016/j.trecan.2020.05.004 |
Senescent Cells In Cancer Therapy: Friends Or
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Wang, Boshi; Kohli, Jaskaren; Demaria, Marco |
Trends In Cancer |
2020 |
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10.1021/acs.jmedchem.8b00506 |
Discovery Of Qca570 As An Exceptionally Potent And
Efficacious Proteolysis Targeting Chimera (Protac) Degrader Of The
Bromodomain And Extra-Terminal (Bet) Proteins Capable Of Inducing
Complete And Durable Tumor Regression |
Qin, Chong; Hu, Yang; Zhou, Bing, 0000-0003-1813-8035;
Fernandez-Salas, Ester; Yang, Chao-Yie; Liu, Liu; Mceachern, Donna;
Przybranowski, Sally; Wang, Mi; Stuckey, Jeanne; Meagher, Jennifer; Bai,
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Fuming; Hu, Jiantao; Xiang, Weiguo; Huang, Liyue; Li, Siwei; Wen, Bo;
Sun, Duxin; Wang, Shaomeng, 0000-0002-8782-6950 |
Journal Of Medicinal Chemistry |
2018 |
| 11059 |
10.1021/acs.jmedchem.8b00909 |
Discovery Of Md-224 As A First-In-Class, Highly Potent,
And Efficacious Proteolysis Targeting Chimera Murine Double Minute 2
Degrader Capable Of Achieving Complete And Durable Tumor Regression |
Li, Yangbing; Yang, Jiuling; Aguilar, Angelo;
Mceachern, Donna; Przybranowski, Sally; Liu, Liu; Yang, Chao-Yie; Wang,
Mi; Han, Xin; Wang, Shaomeng, 0000-0002-8782-6950 |
Journal Of Medicinal Chemistry |
2018 |
| 11061 |
10.1021/acs.jmedchem.8b01413 |
Iterative Design And Optimization Of Initially Inactive
Proteolysis Targeting Chimeras (Protacs) Identify Vz185 As A Potent,
Fast, And Selective Von Hippel<U+2013>Lindau (Vhl) Based Dual
Degrader Probe Of Brd9 And Brd7 |
Zoppi, Vittoria; Hughes, Scott J.; Maniaci, Chiara;
Testa, Andrea, 0000-0002-8973-9711; Gmaschitz, Teresa; Wieshofer,
Corinna; Koegl, Manfred; Riching, Kristin M.; Daniels, Danette L.,
0000-0002-7659-3020; Spallarossa, Andrea; Ciulli, Alessio,
0000-0002-8654-1670 |
Journal Of Medicinal Chemistry |
2018 |
| 11062 |
10.1021/acs.jmedchem.8b01572 |
Discovery Of Erd-308 As A Highly Potent Proteolysis
Targeting Chimera (Protac) Degrader Of Estrogen Receptor (Er) |
Hu, Jiantao; Hu, Biao, 0000-0002-4691-6490; Wang,
Mingliang; Xu, Fuming; Miao, Bukeyan; Yang, Chao-Yie; Wang, Mi; Liu,
Zhaomin; Hayes, Daniel F.; Chinnaswamy, Krishnapriya; Delproposto,
James; Stuckey, Jeanne; Wang, Shaomeng, 0000-0002-8782-6950 |
Journal Of Medicinal Chemistry |
2019 |
| 11063 |
10.1021/acs.jmedchem.8b01631 |
Discovery Of Ard-69 As A Highly Potent Proteolysis
Targeting Chimera (Protac) Degrader Of Androgen Receptor (Ar) For The
Treatment Of Prostate Cancer |
Han, Xin; Wang, Chao; Qin, Chong; Xiang, Weiguo;
Fernandez-Salas, Ester; Yang, Chao-Yie; Wang, Mi; Zhao, Lijie; Xu,
Tianfeng; Chinnaswamy, Krishnapriya; Delproposto, James; Stuckey,
Jeanne; Wang, Shaomeng, 0000-0002-8782-6950 |
Journal Of Medicinal Chemistry |
2019 |
| 11065 |
10.1021/acs.jmedchem.8b01826 |
Highly Selective Ptk2 Proteolysis Targeting Chimeras To
Probe Focal Adhesion Kinase Scaffolding Functions |
Popow, Johannes; Arnhof, Heribert; Bader, Gerd; Berger,
Helmut; Ciulli, Alessio, 0000-0002-8654-1670; Covini, David; Dank,
Christian; Gmaschitz, Teresa; Greb, Peter; Karolyi-Ozguer, Jale; Koegl,
Manfred; Mcconnell, Darryl B.; Pearson, Mark; Rieger, Maria; Rinnenthal,
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Steffen; Trainor, Nicole; Traxler, Elisabeth; Wieshofer, Corinna;
Zoephel, Andreas; Ettmayer, Peter, 0000-0002-8422-2625 |
Journal Of Medicinal Chemistry |
2019 |
| 11067 |
10.1021/acs.jmedchem.9b00516 |
Development Of Multifunctional Histone Deacetylase 6
Degraders With Potent Antimyeloma Activity |
Wu, Hao; Yang, Ka, 0000-0001-8937-7397; Zhang,
Zhongrui; Leisten, Eric D.; Li, Ziyuan; Xie, Haibo; Liu, Jin; Smith,
Kerry A.; Novakova, Zora, 0000-0001-9804-6346; Barinka, Cyril,
0000-0003-2751-3060; Tang, Weiping, 0000-0002-0039-3196 |
Journal Of Medicinal Chemistry |
2019 |
| 11069 |
10.1021/acs.jmedchem.9b00871 |
Potent And Preferential Degradation Of Cdk6 Via
Proteolysis Targeting Chimera Degraders |
Su, Shang, 0000-0003-0228-5380; Yang, Zimo; Gao,
Hongying; Yang, Haiyan; Zhu, Songbiao; An, Zixuan; Wang, Juanjuan; Li,
Qing; Chandarlapaty, Sarat; Deng, Haiteng; Wu, Wei; Rao, Yu,
0000-0002-4356-8531 |
Journal Of Medicinal Chemistry |
2019 |
| 11071 |
10.1021/acs.jmedchem.9b01180 |
Discovery Of A Covalent Inhibitor Of Krasg12C (Amg 510)
For The Treatment Of Solid Tumors |
Lanman, Brian A., 0000-0002-8768-7188; Allen, Jennifer
R.; Allen, John G.; Amegadzie, Albert K.; Ashton, Kate S.; Booker, Shon
K.; Chen, Jian Jeffrey; Chen, Ning; Frohn, Michael J.; Goodman, Guy;
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Vu; Minatti, Ana E.; Nguyen, Thomas T.; Nishimura, Nobuko; Pickrell,
Alexander J.; Reed, Anthony B.; Shin, Youngsook, 0000-0003-3866-354X;
Siegmund, Aaron C.; Tamayo, Nuria A.; Tegley, Christopher M.; Walton,
Mary C.; Wang, Hui-Ling, 0000-0003-2748-5266; Wurz, Ryan P.,
0000-0003-1413-5208; Xue, May; Yang, Kevin C.; Achanta, Pragathi;
Bartberger, Michael D., 0000-0002-5167-3139; Canon, Jude; Hollis, L.
Steven; Mccarter, John D.; Mohr, Christopher; Rex, Karen; Saiki, Anne
Y.; San Miguel, Tisha; Volak, Laurie P.; Wang, Kevin H.; Whittington,
Douglas A., 0000-0002-5946-8543; Zech, Stephan G.; Lipford, J. Russell;
Cee, Victor J., 0000-0002-7714-397X |
Journal Of Medicinal Chemistry |
2019 |
| 11072 |
10.1021/acs.jmedchem.9b01393 |
Discovery Of Highly Potent And Efficient Protac
Degraders Of Androgen Receptor (Ar) By Employing Weak Binding Affinity
Vhl E3 Ligase Ligands |
Han, Xin; Zhao, Lijie; Xiang, Weiguo; Qin, Chong; Miao,
Bukeyan; Xu, Tianfeng; Wang, Mi; Yang, Chao-Yie; Chinnaswamy,
Krishnapriya; Stuckey, Jeanne; Wang, Shaomeng, 0000-0002-8782-6950 |
Journal Of Medicinal Chemistry |
2019 |
| 11073 |
10.1021/acs.jmedchem.9b01530 |
Structure-Based Discovery Of Sd-36 As A Potent,
Selective, And Efficacious Protac Degrader Of Stat3 Protein |
Zhou, Haibin; Bai, Longchuan; Xu, Renqi; Zhao, Yujun,
0000-0003-1035-2272; Chen, Jianyong; Mceachern, Donna; Chinnaswamy,
Krishnapriya; Wen, Bo; Dai, Lipeng; Kumar, Praveen; Yang, Chao-Yie,
0000-0002-5445-0109; Liu, Zhaomin; Wang, Mi; Liu, Liu; Meagher, Jennifer
L.; Yi, Han; Sun, Duxin; Stuckey, Jeanne A.; Wang, Shaomeng,
0000-0002-8782-6950 |
Journal Of Medicinal Chemistry |
2019 |
| 11076 |
10.1021/acs.jmedchem.9b02052 |
Identification Of The Clinical Development Candidate
Mrtx849, A Covalent Krasg12C Inhibitor For The Treatment Of Cancer |
Fell, Jay B., 0000-0002-5770-1225; Fischer, John P.;
Baer, Brian R.; Blake, James F.; Bouhana, Karyn; Briere, David M.;
Brown, Karin D.; Burgess, Laurence E.; Burns, Aaron C.; Burkard, Michael
R.; Chiang, Harrah; Chicarelli, Mark J.; Cook, Adam W.; Gaudino, John
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Hingorani, Gary P.; Hinklin, Ronald J.; Mejia, Macedonio J.; Olson,
Peter; Otten, Jennifer N.; Rhodes, Susan P.; Rodriguez, Martha E.;
Savechenkov, Pavel; Smith, Darin J.; Sudhakar, Niranjan; Sullivan,
Francis X.; Tang, Tony P.; Vigers, Guy P.; Wollenberg, Lance;
Christensen, James G.; Marx, Matthew A., 0000-0003-2351-4787 |
Journal Of Medicinal Chemistry |
2020 |
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10.1021/acscentsci.0c00411 |
Targeted Degradation Of Oncogenic Krasg12C By
Vhl-Recruiting Protacs |
Bond, Michael J.; Chu, Ling; Nalawansha, Dhanusha A.;
Li, Ke; Crews, Craig M., 0000-0002-8456-2005 |
Acs Central Science |
2020 |
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10.1021/acscentsci.9b00713 |
Reversible Spatiotemporal Control Of Induced Protein
Degradation By Bistable Photoprotacs |
Pfaff, Patrick, 0000-0002-9761-2497; Samarasinghe,
Kusal T. G.; Crews, Craig M., 0000-0002-8456-2005; Carreira, Erick M.,
0000-0003-1472-490X |
Acs Central Science |
2019 |
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10.1021/acschembio.8b00692 |
Quantitative Live-Cell Kinetic Degradation And
Mechanistic Profiling Of Protac Mode Of Action |
Riching, Kristin M.; Mahan, Sarah; Corona, Cesear R.;
Mcdougall, Mark; Vasta, James D.; Robers, Matthew B.; Urh, Marjeta;
Daniels, Danette L., 0000-0002-7659-3020 |
Acs Chemical Biology |
2018 |
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10.1021/acschembio.8b01083 |
Covalent Ligand Screening Uncovers A Rnf4 E3 Ligase
Recruiter For Targeted Protein Degradation Applications |
Ward, Carl C.; Kleinman, Jordan I.; Brittain, Scott M.;
Lee, Patrick S., 0000-0002-0517-120X; Chung, Clive Yik Sham; Kim,
Kenneth; Petri, Yana; Thomas, Jason R.; Tallarico, John A.; Mckenna,
Jeffrey M.; Schirle, Markus, 0000-0003-4933-2623; Nomura, Daniel K.,
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Acs Chemical Biology |
2019 |
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10.1021/acschembio.8b01094 |
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Hannah; Dittus, Lars; Bassi, Zuni I., 0000-0003-4309-9656; Hughes,
Sophie E.; Muelbaier, Marcel, 0000-0002-5414-0258; Dai, Han; Smith, Ian
E. D.; Kerr, William J., 0000-0002-1332-785X; Burley, Glenn A.,
0000-0002-4896-113X; Bantscheff, Marcus, 0000-0002-8343-8977; Harling,
John D. |
Acs Chemical Biology |
2019 |
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10.1021/acschembio.9b00092 |
Spr-Measured Dissociation Kinetics Of Protac Ternary
Complexes Influence Target Degradation Rate |
Roy, Michael J.; Winkler, Sandra; Hughes, Scott J.;
Whitworth, Claire; Galant, Michael; Farnaby, William; Rumpel, Klaus;
Ciulli, Alessio, 0000-0002-8654-1670 |
Acs Chemical Biology |
2019 |
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10.1021/acsmedchemlett.9b00597 |
Protac Technology: Opportunities And Challenges |
Gao, Hongying, 0000-0001-5078-1317; Sun, Xiuyun,
0000-0001-9634-2707; Rao, Yu, 0000-0002-4356-8531 |
Acs Medicinal Chemistry Letters |
2020 |
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10.1021/jacs.8b08008 |
Addressing Kinase-Independent Functions Of Fak Via
Protac-Mediated Degradation |
Cromm, Philipp M., 0000-0001-5291-3379; Samarasinghe,
Kusal T. G.; Hines, John; Crews, Craig M., 0000-0002-8456-2005 |
Journal Of The American Chemical Society |
2018 |
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10.1021/jacs.8b10320 |
Enhancing Antiproliferative Activity And Selectivity Of
A Flt-3 Inhibitor By Proteolysis Targeting Chimera Conversion |
Burslem, George M., 0000-0002-2812-983X; Song, Jayoung;
Chen, Xin; Hines, John; Crews, Craig M., 0000-0002-8456-2005 |
Journal Of The American Chemical Society |
2018 |
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10.1021/jacs.9b02822 |
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